892549-43-8 Usage
Description
MF-63 is a potent, selective, and orally active inhibitor of human microsomal prostaglandin E2 synthase-1 (mPGES-1), the terminal enzyme in the biosynthesis of PGE2. It exhibits greater than 1,000-fold selectivity over other prostanoid synthases and is effective in preventing LPS-induced hyperalgesia and pyresis, as well as iodoacetate-induced osteoarthritic pain in guinea pigs or mice expressing human mPGES-1. Importantly, MF-63 does not cause the gastrointestinal toxicity associated with non-selective COX inhibitors, while still significantly suppressing PGE2 synthesis in the stomach.
Uses
Used in Pharmaceutical Industry:
MF-63 is used as an anti-inflammatory agent for its ability to selectively inhibit mPGES-1, thereby reducing PGE2 synthesis and alleviating inflammation without causing gastrointestinal toxicity.
Used in Pain Management:
MF-63 is used as an analgesic agent to prevent LPS-induced hyperalgesia and iodoacetate-induced osteoarthritic pain, providing effective pain relief without the side effects associated with non-selective COX inhibitors.
Used in Cancer Therapy:
MF-63 is used as an anti-cancer agent, leveraging its inhibitory effects on mPGES-1 to potentially impact cancer progression and treatment.
in vitro
mf63 was found to be significantly more potent than those previously reported mpges-1 inhibitors with an intrinsic inhibitory potency on the recombinant human mpges-1 enzyme. furthermore, mf63 showed a pge2 whole cell inhibition in a549 cells and a human whole blood activity [1].
in vivo
in rodent species, mf63 inhibited guinea pig mpges-1 strongly but not the mouse or rat enzyme. when tested in the guinea pig and a knock-in (ki) mouse expressing human mpges-1, mf63 suppressed the synthesis of pge2 selectively, but not other prostaglandins that were inhibitable by nonsteroidal anti-inflammatory drugs (nsaid), yet remaided nsaid-like efficacy at inhibiting lipopolysaccharide-induced hyperalgesia, pyresis, and iodoacetate-induced osteoarthritic pain. additionally, mf63 did not cause nsaid-like gastrointestinal toxic effects, such as mucosal erosions or leakage in the ki mice or nonhuman primates, although mf63 markedly inhibited pge2 synthesis in the ki mouse stomach [1].
IC 50
0.9 and 1.3 nm for pig mpges-1 and human mpges-1
references
[1] xu d,rowland se,clark p,giroux a,cté b,guiral s,salem m,ducharme y,friesen rw,méthot n,mancini j,audoly l,riendeau d. mf63 [2-(6-chloro-1h-phenanthro[9,10-d]imidazol-2-yl)-isophthalonitrile], a selective microsomal prostaglandin e synthase-1 inhibitor, relieves pyresis and pain in preclinical models of inflammation. j pharmacol exp ther.2008 sep;326(3):754-63.
Check Digit Verification of cas no
The CAS Registry Mumber 892549-43-8 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 8,9,2,5,4 and 9 respectively; the second part has 2 digits, 4 and 3 respectively.
Calculate Digit Verification of CAS Registry Number 892549-43:
(8*8)+(7*9)+(6*2)+(5*5)+(4*4)+(3*9)+(2*4)+(1*3)=218
218 % 10 = 8
So 892549-43-8 is a valid CAS Registry Number.